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Fundamentals > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What are the two active transporters?

A

SLC family and ABC family

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2
Q

What is the ABC transporter?

A

it is a primary active transporter and it uses the ATP-Binding Cassette

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3
Q

what is the SLC transporter?

A

it is a secondary active transporter

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4
Q

what are the examples of SLC transporters?

A

SERT (fluoxetine and serotonin)
DAT (cocaine, methylphenidate, and dopamine)
OATs and OCTs (organic cations and anions)

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5
Q

what is the example of ABC transporter?

A

MDR1/P-glycoprotein receptor

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6
Q

what does MDR1/p-glycoprotein receptor pump out of brain tissue?

A

loperamide (anti-diarrhea)
morphine
HIV protease inhibitors
anticancer drugs

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7
Q

what part of liver cells metabolizes drugs?

A

the smooth ER

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8
Q

what are the phase I reactions?

A

these split the drug - hydrolysis, oxidation, reduction, hydroxylation
and the de’s: dealkylation, deamination, desulfuration, dechlorination

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9
Q

what are the phase II reactions?

A

these conjugate the drugs by adding a substrate:
glucuronide, glycine, glutathione, sulfate, methyl, acetate

*SAM and the 3G’s

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10
Q

what are the other names for cytochrome p450?

A

CYP, monoxygenase, mixed function oxidases

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11
Q

what are the three requirements int eh CYP reaction?

A

NADPH, molecular oxygen, and NADPH-cytochrom P450 reductase

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12
Q

what are the substrates and inducers of CYP1A2?

A

substrates: acetaminophen, caffeine, theophylline, warfarin
inducers: smoking, charcoal, cruciferous vegetables

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13
Q

what are the substrates and inducers of CYP2A6?

A

substrates: warfarin, zidovudine
inducers: none

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14
Q

what are the substrates and inducers of CYP2C9?

A

substrates: hexobarbital, trimethadione, tolbutamide, phenytoin, ibuprofen, s-warfarin
inducers: rifampin, barbiturates

**http is

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15
Q

what are the substrates and inducers of CYP2C19?

A

substrates: diazepam, omeprazole, propanolol
inducers: none

**DOP

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16
Q

what are the substrates for CYP2D6?

A

substrates: amytriptyline, codeine, debrisoquin, fluoxetine, hydrocodone, timolol
inducers: none

**Apollo Caught Deanna For Hera this Time

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17
Q

what are the substrates and inducers for CYP2E1

A

substrates: ethanol and acetaminophen
inducers: ethanol, isoniazid

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18
Q

what are the substrates and inducers for CYP3A4?

A

substrates: cortisol, amiodarone, diazepam, erythromycin, diltiazem, testosterone, triazolam, midazolam, verapamil, nifedipine, progesterone
inducers: barbiturates, glucocorticoids, rifampin, phenytoin

**Carter ADores Eureka Daily
Today They Made Very Nifty Progress

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19
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for glucuronidation?

A

conjugating agent: UDP glucuronic acid
functional groups: OH, COOH, NH2
enzyme: glucuronyl transferase
drugs: morphine, acetaminophen, diazepam, digoxin (MADD)

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20
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for glutathione?

A

conjugating agent: glutathione (GSH)
functional groups: arene oxide, epoxide, halogen, NO2
enzyme: GSH S-transferases
drugs: acetaminophen

21
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for sulfation?

A

conjugating agent: PAPS (3’-phosphoadenosine 5’-phosphosulfate)
functional groups: OH, NH2
enzyme: sulfotransferases
drugs: 3-hydroxycoumarin, acetaminophen, ethanol, 3-hydroxyacetanilide, methydopa

22
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for acetylation?

A

conjugating agent: acetyl CoA
functional groups: OH, NH2
enzyme: acetyl transferases
drugs: sulfonamide, histamine, isonaizid, procainamide, clonazepam (SHIP C)

23
Q

what is the conjugative agent, involved functional groups, involved enzyme, and involved drugs for methylation?

A

conjugating agent: S-adenosylmethionine
functional groups: O, N, S
enzymes: catechol-O-methytransferase, thiopurine-S-methyltransferase, phenol-O-methyltransferase, N-methyltransferase
drugs: thiopurine, carbamzepine epoxide

24
Q

what are three examples of receptors induced by drugs?

A

pregnane X receptor, constitutive androstane receptor, aryl hydrocarbon receptor

25
Q

What drug(s) induce(s) aryl hydrocarbon receptor?

A

omeprazole

26
Q

What drug(s) induce(s) constitutive androstane receptor?

A

phenobarbital

27
Q

What drug(s) induce(s) pregnane X receptor?

A

rifampin, atorvastatin

28
Q

what to penicillin and probenacid do when they interact?

A

alter elimination

29
Q

what do divalent cations and fluoroquinolones do when they interact?

A

irritate stomach and impair antibiotic absorption

30
Q

what do EtOH and benzodiazepines do when they interact?

A

toxic

31
Q

warfarin + aspirin/NSAIDS?

A

hemorrhagic risk

32
Q

antiseizure drugs and CYP?

A

if CYP is inhibited, drugs are more effective, if CYP is induced by rifampin, have less effective

33
Q

what do polymorphisms in the CYP2D6 gene cause?

A

decreased metabolism of debrinoquin

34
Q

what do polymorphisms in the CYP2C19 gene cause?

A
  1. decreased clopidogrel activity (it is a prodrug that requires CYP2C19)
  2. increased omeprazole activity (used for gastric ulcers)
  3. increased toxicity of phenytoin
35
Q

what do polymorphisms in the CYP2C9 gene cause?

A

increased activity of S-warfarin, phenyoin, losartan

36
Q

what do polymorphisms in dihydropyrimidine dehydrogenase do?

A

lead to impaired metabolism of 5-flurouracil which can caused fatal neuro-toxicity in slow metabolizers (non P450 phase I enzyme)

37
Q

what do polymorphisms in pseudocholinesterase do?

A

dramatically extend the duration of action of succinylcholine (a non P450 phase I enzyme)

38
Q

what does NAT1 do?

A

N-acetyl transferase 1 acetylates simple aromatic amines

39
Q

what does NAT2 do?

A

N-acetyl transferase 2 acetylates polycyclic amines and other substrates

40
Q

what does a polymorphism in NAT2 do?

A
  1. causes isoniazid to go down minor pathway and produce neurotoxic product
  2. causes procainamide to go down phase I pathways via FMO and produce toxic product
  3. faster ANA appearance (Lupus)
41
Q

what does a polymorphism in thiopurine methyl transferase do?

A

6methylpurine (6MP) goes down different pathways and is coverted to 6-TGN leading to toxicity

42
Q

what does a polymorphism in MDR-1 do?

A

altered plasma levels of antiretroviral and fexofenadine

43
Q

what does a polymorphism in beta2 adrenergic receptors do?

A

rapid desensitization by agonists in veins but increased bronchodilator response

44
Q

what does a polymorphism in arachidonate 5-lipoxygenase do?

A

reduce asthma incidence

45
Q

what does a polymorphism in vitamin K epoxide reductase do?

A

affects sensitivity to warfarin

46
Q

warfarin metabolism and action?

A

polymorphisms in CYP2C9 cause slow warfarin metabolism and therefore increase patient sensitivity to warfarin
warfarin does its job (anticoagulation) by inhibiting vitamin K epoxide reductase - when VKORC is mutated, warfarin can’t bind and inhibit VKORC and no anticoagulative activities

47
Q

inhibitors of CYP450?

A

macrolide anitbiotics (erythromycin and clarithromycin), antifungals (triazole), ritonavir, fluoxetine, nefasodone, cimetidine

48
Q

what does grapefruit juice inhibit?

A

CYP3A4

Fundamentals (11 decks)

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